U69593 [Ligand Id: 1655] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL440765 (U-69593) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI | F | 5.7 | pKd | 1980 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
| ChEMBL | Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI | F | 5.7 | pKd | 1980 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
| ChEMBL | Displacement of [3H]-DADLE from human delta opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 4.9 | pKi | 12540 | nM | Ki | Eur J Med Chem (2012) 50: 44-54 [PMID:22341895] |
| ChEMBL | Displacement of [3H]DADLE from human delta opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 4.9 | pKi | 12540 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
| ChEMBL | Displacement of [3H]DADLE from human recombinant opioid delta receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method | B | 4.92 | pKi | >12000 | nM | Ki | Eur J Med Chem (2015) 92: 531-539 [PMID:25599950] |
| ChEMBL | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis | B | 4.92 | pKi | >12000 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
| ChEMBL | Displacement of [3H]Cl-DPDPE from human DOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| ChEMBL | Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Displacement of [3H]pCl-DPDPE from human delta opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Binding affinity of compound was determined against Opioid receptor delta 1 from a native receptor in guinea pig | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
| ChEMBL | Displacement of radiolabeled DPDPE-Cl from delta opioid receptor in Hartley guinea pig brain | B | 5.87 | pKi | 1358 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| ChEMBL | Binding affinity determined against Opioid receptor delta 1 from human cloned receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
| ChEMBL | Binding affinity towards Opioid receptor delta 1 by the displacement of [125I]-Deltorphin | B | 5.23 | pIC50 | 5844 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 197-200 [PMID:11755353] |
| ChEMBL | Inhibition of [125I]deltorphin binding to human delta opioid receptor from membranes of HEK293 cells | B | 5.24 | pIC50 | 5800 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1141-1145 [PMID:12643930] |
| ChEMBL | Tested for inhibitory concentration against [3H]DPDPE binding at sites of delta-opioid receptor in guinea pig brain membrane | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1994) 37: 2856-2864 [PMID:8071934] |
| ChEMBL | Inhibitory concentration was determined against delta-opioid receptor using [3H]- DPDPE radioligand | B | 5.3 | pIC50 | 4970 | nM | IC50 | J Med Chem (1995) 38: 570-579 [PMID:7853350] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells. | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Displacement of [3H]DPDPE from mouse whole brain DOR | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain without cerebellum | B | 6 | pKi | >1000 | nM | Ki | ACS Med Chem Lett (2014) 5: 868-872 [PMID:25147605] |
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain membranes without cerebellum after 1 hr by liquid scintillation counting analysis | B | 6.41 | pKi | 391 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 268-272 [PMID:23200250] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Displacement of [3H]-U69593 from human kappa opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 8.46 | pKi | 3.5 | nM | Ki | Eur J Med Chem (2012) 50: 44-54 [PMID:22341895] |
| ChEMBL | Displacement of [3H]U69,593 from human recombinant opioid kappa receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method | B | 8.46 | pKi | 3.5 | nM | Ki | Eur J Med Chem (2015) 92: 531-539 [PMID:25599950] |
| ChEMBL | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 8.46 | pKi | 3.5 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
| ChEMBL | Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis | B | 8.46 | pKi | 3.5 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
| ChEMBL | Displacement of [3H]diprenorphine from human KOR expressed in HEK293 cells assessed as inhibition constant incubated for 60 mins by liquid scintillation method | B | 8.57 | pKi | 2.68 | nM | Ki | J Med Chem (2023) 66: 5154-5170 [PMID:36987735] |
| ChEMBL | Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| ChEMBL | Binding affinity towards Wild-type kappa opioid receptor expressed in HEK cells | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2000) 43: 1251-1252 [PMID:10753461] |
| ChEMBL | Binding affinity against opioid receptor kappa 1 from human cloned receptor | B | 8.95 | pKi | 1.11 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
| ChEMBL | Displacement of [3H]U69593 from human KOR expressed in CHO cells | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 666-669 [PMID:28011222] |
| ChEMBL | Displacement of [3H]U69,593 from human kappa opioid receptor transfected in CHO cell membranes after 60 mins | B | 8.98 | pKi | 1.05 | nM | Ki | Bioorg Med Chem (2014) 22: 2508-2516 [PMID:24657054] |
| ChEMBL | Displacement of [3H]U69593 from human KOR expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2021) 64: 9458-9483 [PMID:34152138] |
| ChEMBL | Binding affinity to kappa opioid receptor | B | 9.32 | pKi | 0.47 | nM | Ki | Bioorg Med Chem (2010) 18: 4446-4452 [PMID:20478711] |
| GtoPdb | - | - | 9.5 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Eur J Pharmacol (1985) 109: 281-4 [PMID:2986999] |
| ChEMBL | Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Binding affinity to KOR (unknown origin) assessed as inhibition constant | B | 9.52 | pKi | 0.3 | nM | Ki | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| ChEMBL | Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Displacement of [3H]naloxone from kappa opioid receptor expressed in HEK293 cell membrane | B | 8.1 | pIC50 | 8 | nM | IC50 | J Nat Prod (2010) 73: 988-991 [PMID:20426456] |
| ChEMBL | Displacement of [3H]diprenorphine from human KOR expressed in HEK293 cells incubated for 60 mins by liquid scintillation method | B | 8.17 | pIC50 | 6.69 | nM | IC50 | J Med Chem (2023) 66: 5154-5170 [PMID:36987735] |
| ChEMBL | Binding affinity towards Opioid receptor kappa 1 by the displacement of [125I]-(D-Pro10)-Dynorphin A | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 197-200 [PMID:11755353] |
| ChEMBL | Inhibition of [125I]-(D-Pro10)-Dynorphin A binding to human kappa opioid receptor from membranes of HEK293 cells | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1141-1145 [PMID:12643930] |
| ChEMBL | Agonist activity at human kappa opioid receptor by [35S]GTPgammaS binding assay | F | 6.48 | pEC50 | 330 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6111-6115 [PMID:17904842] |
| ChEMBL | Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 6.68 | pEC50 | 207 | nM | EC50 | J Med Chem (2007) 50: 3596-3603 [PMID:17580847] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding | F | 6.68 | pEC50 | 207 | nM | EC50 | J Nat Prod (2006) 69: 107-112 [PMID:16441078] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with GFP and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 20 mins by Hoechst staining-based assay | B | 6.69 | pEC50 | 205 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by luminescence assay | B | 6.88 | pEC50 | 131 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 7.08 | pEC50 | 83.76 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human recombinant kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 45 mins by microplate luminescence assay | F | 7.1 | pEC50 | 80 | nM | EC50 | J Med Chem (2010) 53: 4212-4222 [PMID:20441176] |
| ChEMBL | Agonist activity at recombinant kappa-opioid receptor in human HEK293 cells by [35S]-GTP-gammaS binding assay | F | 7.1 | pEC50 | 80 | nM | EC50 | Bioorg Med Chem (2014) 22: 3316-3324 [PMID:24856182] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S binding at kappa opioid receptor in human brain cortical membrane | F | 7.19 | pEC50 | 64.3 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3609-3613 [PMID:16650985] |
| ChEMBL | Agonist activity at human kappa opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis | F | 7.22 | pEC50 | 60.14 | nM | EC50 | Bioorg Med Chem (2014) 22: 2508-2516 [PMID:24657054] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cells assessed as induction of beta-arrestin-2 recruitment by enzyme fragment complementation assay | F | 7.28 | pEC50 | 52 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2770-2772 [PMID:29426768] |
| ChEMBL | Agonist activity at KOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay | F | 7.53 | pEC50 | 29.7 | nM | EC50 | J Med Chem (2023) 66: 17138-17154 [PMID:38095323] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay | F | 7.55 | pEC50 | 28.1 | nM | EC50 | Bioorg Med Chem (2015) 23: 6271-6279 [PMID:26346669] |
| ChEMBL | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells after 2 hrs by [35S]-GTPgammaS binding assay | F | 7.55 | pEC50 | 28.1 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 268-272 [PMID:23200250] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.55 | pEC50 | 28.1 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4980-4983 [PMID:25283554] |
| ChEMBL | Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells. | B | 7.58 | pEC50 | 26.1 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay | F | 7.58 | pEC50 | 26.1 | nM | EC50 | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method | F | 7.78 | pEC50 | 16.5 | nM | EC50 | Bioorg Med Chem (2022) 53: 116552-116552 [PMID:34894610] |
| ChEMBL | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as calcium mobilization after 1 hrs by fluorescence analysis | F | 7.9 | pEC50 | 12.5 | nM | EC50 | Bioorg Med Chem (2012) 20: 3100-3110 [PMID:22464684] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding | F | 7.92 | pEC50 | 12 | nM | EC50 | ACS Med Chem Lett (2014) 5: 868-872 [PMID:25147605] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in HEK-293 cells assessed as stimulation of [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting analysis | F | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (2014) 57: 6845-6860 [PMID:25062506] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in HEK-293 cells after 45 mins by [35S]GTP-gamma-S binding assay in presence of 10 uM of GDP | B | 7.92 | pEC50 | 12 | nM | EC50 | Medchemcomm (2016) 7: 317-326 |
| ChEMBL | Agonist activity at KOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay | F | 7.92 | pEC50 | 11.9 | nM | EC50 | J Med Chem (2021) 64: 13394-13409 [PMID:34465090] |
| ChEMBL | Agonist activity at KOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay | F | 7.93 | pEC50 | 11.75 | nM | EC50 | J Med Chem (2021) 64: 13394-13409 [PMID:34465090] |
| ChEMBL | Agonist activity at human kappa opioid receptor in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2008) 51: 4404-4411 [PMID:18637671] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.1 | pEC50 | 8.03 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
| ChEMBL | Agonist activity at KOR (unknown origin) beta-arrestin recruitment signalling in CCL1-induced CHO cells assessed as beta-lactamase level by Tango assay | F | 8.17 | pEC50 | 6.74 | nM | EC50 | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| ChEMBL | Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay | F | 8.18 | pEC50 | 6.6 | nM | EC50 | J Nat Prod (2006) 69: 107-112 [PMID:16441078] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in human U2OS cells assessed as increase in ERK1/2 phosphorylation after 10 mins by Western blot analysis | B | 8.27 | pEC50 | 5.4 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assay | F | 8.28 | pEC50 | 5.3 | nM | EC50 | J Med Chem (2017) 60: 2526-2551 [PMID:28218838] |
| ChEMBL | Agonist activity at KOR (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 60 mins by liquid scintillation counting analysis | B | 8.55 | pEC50 | 2.8 | nM | EC50 | J Med Chem (2021) 64: 9458-9483 [PMID:34152138] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay | F | 8.59 | pEC50 | 2.6 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2770-2772 [PMID:29426768] |
| ChEMBL | Agonist activity at human kappa opioid receptor assessed as inhibition of Galpha-16-induced calcium flux | F | 8.65 | pEC50 | 2.25 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6111-6115 [PMID:17904842] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay | F | 9.1 | pEC50 | 0.8 | nM | EC50 | J Med Chem (2014) 57: 10464-10475 [PMID:25426797] |
| ChEMBL | Agonist activity at KOR (unknown origin) by measuring cAMP inhibition | F | 9.49 | pEC50 | 0.32 | nM | EC50 | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| κ receptor in Mouse [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| GtoPdb | - | - | 8.6 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1993) 90: 6736-40 [PMID:8393575] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Binding affinity to rat kappa opioid receptor expressed in HEK293 cell membranes | B | 9 | pKd | 1 | nM | Kd | Bioorg Med Chem (2015) 23: 3948-3956 [PMID:25593096] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in Wistar rat brain membranes by liquid scintillation counting based competition binding assay | B | 8.24 | pKi | 5.7 | nM | Ki | ACS Med Chem Lett (2014) 5: 1032-1036 [PMID:25221662] |
| ChEMBL | Displacement of [3H]U-69,593 from kappa opioid receptor in rat brain after 60 mins by liquid scintillation counting method | B | 8.4 | pKi | 3.98 | nM | Ki | Bioorg Med Chem (2017) 25: 2406-2422 [PMID:28314512] |
| ChEMBL | Binding constant against E203Q,D204N,D206N,E209Q EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2000) 43: 1251-1252 [PMID:10753461] |
| ChEMBL | Binding constant against E203Q,D204N,D206N EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (2000) 43: 1251-1252 [PMID:10753461] |
| ChEMBL | Binding constant against D216N,D217N,E218Q EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2000) 43: 1251-1252 [PMID:10753461] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Biochem J (1993) 295 ( Pt 3): 625-8 [PMID:8240267]; Proc Natl Acad Sci USA (1993) 90: 9954-8 [PMID:8234341] |
| ChEMBL | Binding constant against wild type EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2000) 43: 1251-1252 [PMID:10753461] |
| ChEMBL | Binding affinity against rat kappa-opioid receptor expressed in CHO cells was determined by competitive inhibition of 2 nM [3H]-U 69593 | B | 9.2 | pIC50 | 0.63 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2027-2032 [PMID:9873480] |
| ChEMBL | Agonist activity at rat kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.11 | pEC50 | 7.7 | nM | EC50 | ACS Med Chem Lett (2014) 5: 1032-1036 [PMID:25221662] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI | F | 5.31 | pKd | 4894 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
| ChEMBL | Binding affinity against kappa opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6 nM nor-BNI | F | 5.31 | pKd | 4894 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
| ChEMBL | Binding affinity at Opioid receptor kappa 1 in guinea pig brain membrane determined by using [3H]U-69593 as radioligand | B | 8.37 | pKd | 4.3 | nM | Kd | J Med Chem (1988) 31: 2015-2021 [PMID:2845084] |
| ChEMBL | Binding affinity for the Opioid receptor kappa 1 | B | 8.14 | pKi | 7.3 | nM | Ki | J Med Chem (1988) 31: 831-836 [PMID:2832603] |
| ChEMBL | Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Binding affinity determined against Opioid receptor kappa 1 from a native receptor in guinea pig | B | 8.72 | pKi | 1.89 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
| ChEMBL | Binding affinity against Opioid receptor kappa 1 in guinea pig. | B | 8.75 | pKi | 1.78 | nM | Ki | J Med Chem (1996) 39: 860-872 [PMID:8632410] |
| ChEMBL | Displacement of [3H]U-69593 from guinea pig cerebellum KOR | B | 8.86 | pKi | 1.37 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | B | 8.86 | pKi | 1.37 | nM | Ki | ACS Med Chem Lett (2014) 5: 868-872 [PMID:25147605] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum after 1 hr by liquid scintillation counting analysis | B | 8.86 | pKi | 1.37 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 268-272 [PMID:23200250] |
| ChEMBL | Tested for inhibitory effect on binding of [3H]bremazocine to opioid receptor kappa in guinea pig cerebellum membranes | B | 8.97 | pKi | 1.06 | nM | Ki | J Med Chem (1992) 35: 4638-4639 [PMID:1361580] |
| ChEMBL | Displacement of [3H]U-69,593 from KOR in guinea pig brain membranes after 120 mins by scintillation counting method | B | 9.01 | pKi | 0.97 | nM | Ki | J Med Chem (2019) 62: 893-907 [PMID:30543421] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane after 150 mins by scintillation counting | B | 9.01 | pKi | 0.97 | nM | Ki | J Med Chem (2010) 53: 4212-4222 [PMID:20441176] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis | B | 9.01 | pKi | 0.97 | nM | Ki | J Med Chem (2014) 57: 6845-6860 [PMID:25062506] |
| ChEMBL | Displacement of [3H]U-69,593 from kappa-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting | B | 9.01 | pKi | 0.97 | nM | Ki | J Med Chem (2017) 60: 2526-2551 [PMID:28218838] |
| ChEMBL | Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 9.01 | pKi | 0.97 | nM | Ki | Medchemcomm (2016) 7: 2368-2380 |
| ChEMBL | Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membarnes by liquid scintillation counting method | B | 9.01 | pKi | 0.97 | nM | Ki | Medchemcomm (2016) 7: 317-326 |
| ChEMBL | Displacement of [3H]U-69593 from kappa-opioid receptor in guinea pig brain membrane | B | 9.06 | pKi | 0.88 | nM | Ki | Bioorg Med Chem (2014) 22: 3316-3324 [PMID:24856182] |
| ChEMBL | Displacement of radiolabeled U69593 from kappa1 opioid receptor in Hartley guinea pig brain | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| ChEMBL | Tested for inhibitory concentration against [3H]U-69593 binding at sites of kappa-opioid receptor in guinea pig brain membrane | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (1994) 37: 2856-2864 [PMID:8071934] |
| ChEMBL | Inhibitory concentration against Opioid receptor kappa 1 using [3H]- U-69,593 radioligand | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (1995) 38: 570-579 [PMID:7853350] |
| ChEMBL | Agonist activity at KOR in guinea pig brain membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting analysis | F | 5.84 | pEC50 | 1445.44 | nM | EC50 | ACS Med Chem Lett (2022) 13: 1707-1714 [PMID:36385929] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from human MOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 5.63 | pKi | 2370 | nM | Ki | Eur J Med Chem (2013) 67: 335-343 [PMID:23880358] |
| ChEMBL | Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting | B | 5.63 | pKi | 2370 | nM | Ki | Eur J Med Chem (2012) 50: 44-54 [PMID:22341895] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis | B | 5.7 | pKi | >2000 | nM | Ki | Bioorg Med Chem (2013) 21: 3298-3309 [PMID:23618710] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant opioid mu receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method | B | 5.7 | pKi | >2000 | nM | Ki | Eur J Med Chem (2015) 92: 531-539 [PMID:25599950] |
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting | B | 5.94 | pKi | 1145 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. | B | 5.94 | pKi | 1145 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Binding affinity determined against Opioid receptor mu 1 from human cloned receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
| ChEMBL | Inhibition of [125I]Enkephalin binding to human mu opioid receptor from membranes of HEK293 cells | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1141-1145 [PMID:12643930] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 by the displacement of [125I]Enkephalin; Not determined | B | 6.61 | pIC50 | 248 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 197-200 [PMID:11755353] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mouse whole brain MOR | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum | B | 6 | pKi | >1000 | nM | Ki | ACS Med Chem Lett (2014) 5: 868-872 [PMID:25147605] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain membranes without cerebellum after 1 hr by liquid scintillation counting analysis | B | 6.26 | pKi | 548 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 268-272 [PMID:23200250] |
| ChEMBL | Binding affinity against opioid receptor by displacing radioligand [3HlU69,593 | B | 8.93 | pKi | 1.18 | nM | Ki | J Med Chem (1994) 37: 3408-3418 [PMID:7932569] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane | B | 5.14 | pKi | 7250 | nM | Ki | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6000 nM CTAP | F | 5.67 | pKd | 2142 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
| ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 6000 nM CTAP | F | 5.67 | pKd | 2142 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
| ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | F | 6.16 | pKd | 684 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
| ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | F | 6.16 | pKd | 684 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
| ChEMBL | Binding affinity of compound was determined against Opioid receptor mu 1 from native receptor in guinea pig | B | 5.73 | pKi | 1880 | nM | Ki | J Med Chem (2003) 46: 3853-3864 [PMID:12930147] |
| ChEMBL | Displacement of radiolabeled DAMGO from mu opioid receptor in Hartley guinea pig brain | B | 6.16 | pKi | 692 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| ChEMBL | Tested for inhibitory effect on binding of [3H]DAMGO to opioid receptor mu in guinea pig cerebellum membranes | B | 6.26 | pKi | 551 | nM | Ki | J Med Chem (1992) 35: 4638-4639 [PMID:1361580] |
| ChEMBL | Binding affinity for the Opioid receptor mu 1 | B | 7.28 | pKi | 52 | nM | Ki | J Med Chem (1988) 31: 831-836 [PMID:2832603] |
| ChEMBL | Tested for inhibitory concentration against [3H]DAMGO binding at sites of mu-opioid receptor in guinea pig brain membrane | B | 5.75 | pIC50 | 1760 | nM | IC50 | J Med Chem (1994) 37: 2856-2864 [PMID:8071934] |
| ChEMBL | Inhibitory concentration was determined against Opioid receptor mu 1 using [3H]- DAMGO radioligand | B | 5.75 | pIC50 | 1760 | nM | IC50 | J Med Chem (1995) 38: 570-579 [PMID:7853350] |
| NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
| ChEMBL | Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| Nociceptin receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5492] [UniProtKB: P47748] | ||||||||
| ChEMBL | Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain | B | 5.96 | pKi | 1099 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4291-4295 [PMID:16777416] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 4.7 | pIC50 | 19952.62 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
